Assay Detail
Binding
CHEMBL5133797
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Inhibition of BTK (unknown origin)
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 8.03 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5188786 | — | — | 1 | 9.66 |
| CHEMBL5192152 | — | — | 1 | 9.40 |
| CHEMBL5188750 | — | — | 1 | 9.36 |
| CHEMBL5173641 | — | — | 1 | 9.36 |
| CHEMBL5197926 | — | — | 1 | 9.19 |
| CHEMBL5170448 | — | — | 1 | 9.16 |
| CHEMBL5197765 | — | — | 1 | 9.08 |
| CHEMBL5186635 | — | — | 1 | 9.01 |
| CHEMBL5189116 | — | — | 1 | 9.00 |
| CHEMBL5200748 | — | — | 1 | 9.00 |
| CHEMBL5188545 | — | — | 1 | 9.00 |
| CHEMBL4483575 | REMIBRUTINIB | 3.0 | 1 | 8.92 |
| CHEMBL5182804 | — | — | 1 | 8.92 |
| CHEMBL5180944 | — | — | 1 | 8.87 |
| CHEMBL5204339 | — | — | 1 | 8.80 |
| CHEMBL5189311 | — | — | 1 | 8.54 |
| CHEMBL5170218 | — | — | 1 | 8.52 |
| CHEMBL5169775 | — | — | 1 | 8.52 |
| CHEMBL5204655 | — | — | 1 | 8.52 |
| CHEMBL5170919 | — | — | 1 | 8.40 |
| CHEMBL5172575 | — | — | 1 | 8.32 |
| CHEMBL5208570 | — | — | 1 | 8.15 |
| CHEMBL5192675 | — | — | 1 | 8.15 |
| CHEMBL5207196 | — | — | 1 | 8.15 |
| CHEMBL5180966 | — | — | 1 | 7.96 |
| CHEMBL5179299 | — | — | 1 | 7.92 |
| CHEMBL5207026 | — | — | 1 | 7.77 |
| CHEMBL5179923 | — | — | 1 | 7.55 |
| CHEMBL5207401 | — | — | 1 | 7.50 |
| CHEMBL5208901 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5188786 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL5192152 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5173641 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5188750 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5197926 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL5170448 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL5197765 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL5186635 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL5189116 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5200748 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5188545 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4483575 | REMIBRUTINIB | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5182804 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5180944 | — | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL5204339 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5189311 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5170218 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5169775 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5204655 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5170919 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5172575 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5192675 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5207196 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5208570 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5180966 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5179299 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5207026 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5179923 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5207401 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5208901 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5178185 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5173824 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL5195259 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5184493 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5206619 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL5207396 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL5203006 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5191642 | — | IC50 | = | 1716.0 | nM | 5.76 |
| CHEMBL5188454 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5201075 | — | IC50 | = | 7300.0 | nM | 5.14 |